CN101969973B - 组织蛋白酶b抑制剂 - Google Patents

组织蛋白酶b抑制剂 Download PDF

Info

Publication number: CN101969973B
Authority: CN; China
Prior art keywords: tert; base; pyrrolidine; cyclopropylamino; formula
Prior art date: 2008-02-07
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Expired - Fee Related

Application number

CN200980109079.9A

Other languages

English (en)

Chinese (zh)

Other versions

CN101969973A (zh

Inventor

莱斯利·霍尔辛格

Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Virobay Inc

Original Assignee

Virobay Inc

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2008-02-07

Filing date

2009-02-05

Publication date

2015-07-22

2009-02-05 Application filed by Virobay Inc filed Critical Virobay Inc

2011-02-09 Publication of CN101969973A publication Critical patent/CN101969973A/zh

2015-07-22 Application granted granted Critical

2015-07-22 Publication of CN101969973B publication Critical patent/CN101969973B/zh

Status Expired - Fee Related legal-status Critical Current

2029-02-05 Anticipated expiration legal-status Critical

Links

0 CC*[C@@](*)NC([C@](C[C@@](*CC*)C1)N1C(C1(**)CC1)=O)=O Chemical compound CC*[C@@](*)NC([C@](C[C@@](*CC*)C1)N1C(C1(**)CC1)=O)=O 0.000 description 5
QIFVYIVGMIOTJC-DOMZBBRYSA-N CC(C)(C)OC(N(C[C@@H](C1)Oc2nc(-c3ncccc3)nc3c2cc[s]3)[C@@H]1C(O)=O)=O Chemical compound CC(C)(C)OC(N(C[C@@H](C1)Oc2nc(-c3ncccc3)nc3c2cc[s]3)[C@@H]1C(O)=O)=O QIFVYIVGMIOTJC-DOMZBBRYSA-N 0.000 description 1
MZMNEDXVUJLQAF-YUMQZZPRSA-N CC(C)(C)OC(N(C[C@H](C1)O)[C@@H]1C(OC)=O)=O Chemical compound CC(C)(C)OC(N(C[C@H](C1)O)[C@@H]1C(OC)=O)=O MZMNEDXVUJLQAF-YUMQZZPRSA-N 0.000 description 1
FBGKHCCKXVRREA-QTZVNIFKSA-N CC(C)(C)[C@@H](C(N(C[C@@H](C1)Oc(cc2)ncc2Cl)[C@@H]1C(N[C@@H](CC1CCC1)C(C(NC1CC1)=O)=O)=O)=O)NC(OC(C)(C)C)=O Chemical compound CC(C)(C)[C@@H](C(N(C[C@@H](C1)Oc(cc2)ncc2Cl)[C@@H]1C(N[C@@H](CC1CCC1)C(C(NC1CC1)=O)=O)=O)=O)NC(OC(C)(C)C)=O FBGKHCCKXVRREA-QTZVNIFKSA-N 0.000 description 1
PKBCCOYLTICKIY-SRGWINKKSA-N CCC[C@@H](C(C(NC1CC1)=O)=O)NC([C@H](C[C@H](C1)Oc2c(ccc(OCC)c3)c3ccn2)N1C([C@H](C(C)(C)C)NC(NC(C)(C)C)=O)=O)=O Chemical compound CCC[C@@H](C(C(NC1CC1)=O)=O)NC([C@H](C[C@H](C1)Oc2c(ccc(OCC)c3)c3ccn2)N1C([C@H](C(C)(C)C)NC(NC(C)(C)C)=O)=O)=O PKBCCOYLTICKIY-SRGWINKKSA-N 0.000 description 1
DGGJQLCAYQCPDD-UHFFFAOYSA-N COC(c1c(N)[s]cc1)=O Chemical compound COC(c1c(N)[s]cc1)=O DGGJQLCAYQCPDD-UHFFFAOYSA-N 0.000 description 1
CBIDWCOAELWUSK-UHFFFAOYSA-N Oc1nc(-c2cccc[n]2)nc2c1cc[s]2 Chemical compound Oc1nc(-c2cccc[n]2)nc2c1cc[s]2 CBIDWCOAELWUSK-UHFFFAOYSA-N 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/05—Dipeptides
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system

Landscapes

Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Bioinformatics & Cheminformatics (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Neurology (AREA)
Physical Education & Sports Medicine (AREA)
Biomedical Technology (AREA)
Rheumatology (AREA)
Neurosurgery (AREA)
Orthopedic Medicine & Surgery (AREA)
Immunology (AREA)
Gastroenterology & Hepatology (AREA)
Virology (AREA)
Dermatology (AREA)
Oncology (AREA)
Epidemiology (AREA)
Proteomics, Peptides & Aminoacids (AREA)
Addiction (AREA)
Psychiatry (AREA)
Diabetes (AREA)
Molecular Biology (AREA)
Hematology (AREA)
Hospice & Palliative Care (AREA)
Ophthalmology & Optometry (AREA)
Heart & Thoracic Surgery (AREA)
Obesity (AREA)
Pain & Pain Management (AREA)
Urology & Nephrology (AREA)
Cardiology (AREA)

CN200980109079.9A 2008-02-07 2009-02-05 组织蛋白酶b抑制剂 Expired - Fee Related CN101969973B (zh)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US2700708P	2008-02-07	2008-02-07
US61/027,007		2008-02-07
PCT/US2009/033229 WO2009100225A1 (en)	2008-02-07	2009-02-05	Inhibitors of cathepsin b

Publications (2)

Publication Number	Publication Date
CN101969973A CN101969973A (zh)	2011-02-09
CN101969973B true CN101969973B (zh)	2015-07-22

Family

ID=40939419

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
CN200980109079.9A Expired - Fee Related CN101969973B (zh)	2008-02-07	2009-02-05	组织蛋白酶b抑制剂

Country Status (9)

Country	Link
US (1)	US8211897B2 (sr)
EP (1)	EP2237793A4 (sr)
JP (2)	JP5718647B2 (sr)
CN (1)	CN101969973B (sr)
BR (1)	BRPI0907729A2 (sr)
CA (1)	CA2713108A1 (sr)
EA (1)	EA201001262A1 (sr)
MX (1)	MX2010008371A (sr)
WO (1)	WO2009100225A1 (sr)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
WO2008141227A1 (en)	2007-05-10	2008-11-20	Intermune, Inc.	Novel peptide inhibitors of hepatitis c virus replication
EA201071034A1 (ru)	2008-04-15	2011-06-30	Интермьюн, Инк.	Новые макроциклические ингибиторы репликаций вируса гепатита с
AR075584A1 (es)	2009-02-27	2011-04-20	Intermune Inc	COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
CA2854569A1 (en) *	2011-11-25	2013-05-30	David Banner	Novel pyrrolidine derivatives as inhibitors of cathepsin
US20140256698A1 (en) *	2013-03-11	2014-09-11	Virobay, Inc.	Cathepsin inhibitors
SG11201804901WA (en)	2015-12-22	2018-07-30	SHY Therapeutics LLC	Compounds for the treatment of cancer and inflammatory disease
PL3472149T3 (pl)	2016-06-21	2024-02-12	Orion Ophthalmology LLC	Heterocykliczne pochodne prolinamidu
US10526315B2 (en)	2016-06-21	2020-01-07	Orion Ophthalmology LLC	Carbocyclic prolinamide derivatives
CN109661389A (zh) *	2016-08-23	2019-04-19	豪夫迈·罗氏有限公司	作为htra1抑制剂的新型二氟酮酰胺衍生物
US10834908B2 (en) *	2017-04-26	2020-11-17	InfiCure Bio AB	Model animal for fibrosis
EA201992780A1 (ru)	2017-06-21	2020-06-02	ШАЙ ТЕРАПЬЮТИКС ЭлЭлСи	Соединения, которые взаимодействуют с суперсемейством ras, для лечения рака, воспалительных заболеваний, ras-опатий и фиброзного заболевания
CA3069701A1 (en) *	2017-07-17	2019-01-24	The Regents Of The University Of Colorado	Compositions and methods for preventing and treating radiation-induced bystander effects caused by radiation or radiotherapy
US12391705B2 (en)	2018-12-19	2025-08-19	Shy Therapeutics, Llc	Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease

Citations (1)

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Publication number	Priority date	Publication date	Assignee	Title
US20070054864A1 (en) *	2005-06-30	2007-03-08	Michael Graupe	HCV Inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP1028964A1 (en) *	1997-11-11	2000-08-23	Pfizer Products Inc.	Thienopyrimidine and thienopyridine derivatives useful as anticancer agents
US6404397B1 (en)	1998-08-10	2002-06-11	Raytheon Company	Compact all-weather electromagnetic imaging system
US6323180B1 (en) *	1998-08-10	2001-11-27	Boehringer Ingelheim (Canada) Ltd	Hepatitis C inhibitor tri-peptides
US6608027B1 (en) *	1999-04-06	2003-08-19	Boehringer Ingelheim (Canada) Ltd	Macrocyclic peptides active against the hepatitis C virus
AU2001228811A1 (en) *	2000-01-26	2001-08-07	Ono Pharmaceutical Co. Ltd.	Nitrogen-containing 5-membered cyclic compounds and drugs containing these compounds as the active ingredient
CA2369970A1 (en) *	2002-02-01	2003-08-01	Boehringer Ingelheim (Canada) Ltd.	Hepatitis c inhibitor tri-peptides
ES2361997T3 (es)	2003-09-22	2011-06-27	Boehringer Ingelheim International Gmbh	Péptidos macrocíclicos activos contra el virus de la hepatitis c.
WO2006113942A2 (en)	2005-04-20	2006-10-26	Schering Corporation	Method of inhibiting cathepsin activity
WO2006130552A2 (en)	2005-06-02	2006-12-07	Schering Corporation	Methods of treating hepatitis c virus
US20060287248A1 (en)	2005-06-02	2006-12-21	Schering Corporation	Asymmetric dosing methods
US20060276407A1 (en) *	2005-06-02	2006-12-07	Schering Corporation	Methods of treating hepatitis C virus
KR20090024834A (ko) *	2006-07-05	2009-03-09	인터뮨, 인크.	Ｃ형 간염 바이러스 복제의 신규 억제제
US20080161254A1 (en)	2007-01-03	2008-07-03	Virobay, Inc.	Hcv inhibitors

2009
- 2009-02-05 WO PCT/US2009/033229 patent/WO2009100225A1/en not_active Ceased
- 2009-02-05 EP EP09709414.8A patent/EP2237793A4/en not_active Withdrawn
- 2009-02-05 EA EA201001262A patent/EA201001262A1/ru unknown
- 2009-02-05 MX MX2010008371A patent/MX2010008371A/es active IP Right Grant
- 2009-02-05 US US12/366,504 patent/US8211897B2/en not_active Expired - Fee Related
- 2009-02-05 JP JP2010545997A patent/JP5718647B2/ja active Active
- 2009-02-05 CN CN200980109079.9A patent/CN101969973B/zh not_active Expired - Fee Related
- 2009-02-05 BR BRPI0907729-4A patent/BRPI0907729A2/pt not_active IP Right Cessation
- 2009-02-05 CA CA2713108A patent/CA2713108A1/en not_active Abandoned
2014
- 2014-10-10 JP JP2014209108A patent/JP2015051985A/ja not_active Withdrawn

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20070054864A1 (en) *	2005-06-30	2007-03-08	Michael Graupe	HCV Inhibitors

Also Published As

Publication number	Publication date
WO2009100225A1 (en)	2009-08-13
EA201001262A1 (ru)	2011-04-29
CN101969973A (zh)	2011-02-09
JP5718647B2 (ja)	2015-05-13
BRPI0907729A2 (pt)	2015-07-14
JP2015051985A (ja)	2015-03-19
EP2237793A1 (en)	2010-10-13
MX2010008371A (es)	2010-10-04
US20090203629A1 (en)	2009-08-13
US8211897B2 (en)	2012-07-03
JP2011511089A (ja)	2011-04-07
CA2713108A1 (en)	2009-08-13
EP2237793A4 (en)	2013-07-31

Legal Events

Date	Code	Title	Description
2011-02-09	C06	Publication
2011-02-09	PB01	Publication
2011-03-23	C10	Entry into substantive examination
2011-03-23	SE01	Entry into force of request for substantive examination
2015-07-22	C14	Grant of patent or utility model
2015-07-22	GR01	Patent grant
2017-03-29	CF01	Termination of patent right due to non-payment of annual fee
2017-03-29	CF01	Termination of patent right due to non-payment of annual fee	Granted publication date: 20150722 Termination date: 20160205

Publication	Publication Date	Title
CN101969973B (zh)	2015-07-22	组织蛋白酶b抑制剂
JP5368089B2 (ja)	2013-12-18	Ｈｃｖインヒビター
EP2729443B1 (en)	2015-11-25	Benzylamine derivatives as inhibitors of plasma kallikrein
BRPI0708524A2 (pt)	2011-05-31	compostos de n-formil hidroxilamina
US6515011B2 (en)	2003-02-04	Thrombin inhibitors
KR20090086619A (ko)	2009-08-13	2-[6-(3-아미노-피페리딘-1-일)-3-메틸-2,4-디옥소-3,4-디하이드로-2ｈ-피리미딘-1-일메틸]-4-플루오로-벤조니트릴 숙신산염의 다형체 및 그의 이용 방법
JP2008505976A (ja)	2008-02-28	テトラペプチド類似体
JP2021519312A (ja)	2021-08-10	カルパインモジュレーター及びその治療的使用
JP2024097099A (ja)	2024-07-18	Ｍｍｐ７阻害作用を有するペプチドコンジュゲート
US7067491B2 (en)	2006-06-27	Heterocyclic compounds having elastase-inhibiting activity and intermediates thereof
US6417161B1 (en)	2002-07-09	Amino acid amidinohydrazones, alkoxyguanidines and aminoguanidines as protease inhibitors
JP2004507539A (ja)	2004-03-11	ピロリジン誘導体及びそのキマーゼ阻害剤としての使用
CN101242816A (zh)	2008-08-13	Hcv抑制剂
US7084134B2 (en)	2006-08-01	Thrombin inhibitors
JP2003231645A (ja)	2003-08-19	ピロリジン誘導体からなる医薬
HK1197055B (en)	2016-11-04	Benzylamine derivatives as inhibitors of plasma kallikrein